380449-54-7
中文名稱
MELFLUFEN HYDROCHLORIDE
英文名稱
Nelotanserin
CAS
380449-54-7
分子式
C24H31Cl3FN3O3
分子量
534.88
MOL 文件
380449-54-7.mol
更新日期
2024/11/19 11:42:46
380449-54-7 結(jié)構(gòu)式
基本信息
英文別名
Melflufen hydrochlorideethyl (2S)-2-[[(2S)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-3-(4-fluorophenyl)propanoate
常見問題列表
生物活性
Melflufen (Melphalan flufenamide) hydrochloride，Melphalan 的一種二肽前體藥物，是一種烷基化劑。Melflufen hydrochloride 對(duì)多發(fā)性骨髓瘤細(xì)胞具有抗腫瘤活性，并抑制血管生成。Melflufen hydrochloride 對(duì)骨髓瘤細(xì)胞 DNA 不可逆損傷及細(xì)胞毒作用。體外研究
Melflufen (Melphalan flufenamide) hydrochloride (0.5-10 μM; 24 hours) decreases viability of MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, and ANBL-6 cells in a concentration-dependent manner.
Melflufen hydrochloride induces apoptosis in MM.1S cells.
Melflufen hydrochloride also is a potent activator of exosome secretion.
Cell Viability Assay
| Cell Line: | Multiple myeloma cells: MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, ANBL-6 cells |
| Concentration: | 0.5, 1, 3, 5, 10 μM |
| Incubation Time: | 24 hours |
| Result: | A significant concentration-dependent decrease in viability of all cell lines was observed. |
體內(nèi)研究
Melflufen (Melphalan flufenamide) hydrochloride (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model.
| Animal Model: | CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model) |
| Dosage: | 3 mg/kg |
| Administration: | 1.v.; twice-weekly for two weeks |
| Result: | Significantly inhibited MM tumor growth and prolonged survival of mice. |